J Appl Biomed 5:25-30, 2007 | DOI: 10.32725/jab.2007.004

In vitro reactivation potency of bispyridinium (E)-but-2-ene linked acetylcholinesterase reactivators against tabun-inhibited acetylcholinesterase

Kamil Musílek1,3,*, Kamil Kuča1,2, Daniel Jun1,2, Martin Doležal3
1 Department of Toxicology, Faculty of Military Health Sciences, Hradec Králové, Czech Republic
2 Centre of Advanced Studies, Faculty of Military Health Sciences, Hradec Králové, Czech Republic
3 Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic

Six potential bispyridinium (E)-but-2-ene linked AChE reactivators were tested on tabun-inhibited acetylcholinesterase in vitro. Their reactivation efficacy was compared to currently available AChE reactivators used in the case of organophosphorus intoxications - pralidoxime, HI-6 and obidoxime. According to the results obtained, (E)-1,4'-bis(4-hydroxyiminomethylpyridinium)but-2-ene dibromide (K075) seems to be the most potent reactivator of tabun-inhibited AChE. From the data, the reactivation potency of these compounds depends on structural factors such as the constitution of the linking chain between both pyridinium rings and the position of the oxime moiety at the pyridinium rings.

Keywords: organophosphate; tabun; acetylcholinesterase; reactivation; oxime

Received: October 10, 2006; Published: March 31, 2007  Show citation

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Musílek K, Kuča K, Jun D, Doležal M. In vitro reactivation potency of bispyridinium (E)-but-2-ene linked acetylcholinesterase reactivators against tabun-inhibited acetylcholinesterase. J Appl Biomed. 2007;5(1):25-30. doi: 10.32725/jab.2007.004.
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